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Quantitative Structure-Activity Relationship

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Artificial intelligence to predict inhibitors of drug-metabolizing enzymes and transporters for safer drug design.

Expert opinion on drug discovery
INTRODUCTION: Drug-metabolizing enzymes (DMEs) and transporters (DTs) play integral roles in drug metabolism and drug-drug interactions (DDIs) which directly impact drug efficacy and safety. It is well-established that inhibition of DMEs and DTs ofte...

Improved QSAR methods for predicting drug properties utilizing topological indices and machine learning models.

The European physical journal. E, Soft matter
This research investigates the anticipated physicochemical and topological properties of compounds such as drug complexity (C), molecular weight (MW), and topological polar surface area (TPSA) using quantitative structure-activity relationship (QSAR)...

Combining Machine Learning and Electrophysiology for Insect Odorant Receptor Studies.

Methods in molecular biology (Clifton, N.J.)
Insects rely on olfaction in many aspects of their life, and odorant receptors are key proteins in this process. Whereas a plethora of insect odorant receptor sequences is available, most of them are still orphan or uncompletely characterized, since ...

Prediction of plasma concentration-time profiles in mice using deep neural network integrated with pharmacokinetic models.

International journal of pharmaceutics
Quantitative structure-activity relationship (QSAR) methods have emerged as powerful tools to streamline non-clinical pharmacokinetic (PK) studies, with extensive evidence demonstrating their potential to predict key in vivo PK parameters such as cle...

Computational screening of natural products as tryptophan 2,3-dioxygenase inhibitors: Insights from CNN-based QSAR, molecular docking, ADMET, and molecular dynamics simulations.

Computers in biology and medicine
Parkinson's disease (PD) is characterised by a complex array of motor, psychiatric, and gastrointestinal symptoms, many of which are linked to disruptions in neuroactive metabolites. Dysregulated activity of tryptophan 2,3-dioxygenase (TDO), a key en...

Machine learning-driven insights into retention mechanism in IAM chromatography of anticancer sulfonamides: Implications for biological efficacy.

Journal of chromatography. A
Machine learning (ML) tools offer new opportunities in drug discovery, especially for enhancing our understanding of molecular interactions with biological systems. This study develops a comprehensive quantitative structure-retention relationship (QS...

PoseidonQ: A Free Machine Learning Platform for the Development, Analysis, and Validation of Efficient and Portable QSAR Models for Drug Discovery.

Journal of chemical information and modeling
The advent of powerful machine learning algorithms as well as the availability of high volume of pharmacological data has given new fuel to QSAR, opening new unprecedented options for deriving highly predictive models for assisting the rationale desi...

Machine Learning-Assisted Molecular Structure Embedding for Accurate Prediction of Emerging Contaminant Removal by Ozonation Oxidation.

Environmental science & technology
Ozone has demonstrated high efficacy in depredating emerging contaminants (ECs) during drinking water treatment. However, traditional quantitative structure-activation relationship (QSAR) models often fall short in effectively normalizing and charact...

Predicting biomolecule adsorption on nanomaterials: a hybrid framework of molecular simulations and machine learning.

Nanoscale
The adsorption of biomolecules on the surface of nanomaterials (NMs) is a critical determinant of their behavior, toxicity, and efficacy in biological systems. Experimental testing of these phenomena is often costly or complicated. Computational appr...

Machine-Learning Framework to Predict the Performance of Lipid Nanoparticles for Nucleic Acid Delivery.

ACS applied bio materials
Lipid nanoparticles (LNPs) are highly effective carriers for gene therapies, including mRNA and siRNA delivery, due to their ability to transport nucleic acids across biological membranes, low cytotoxicity, improved pharmacokinetics, and scalability....